基于喹唑啉的α1-肾上腺素能受体荧光探针的发现。
Discovery of Quinazoline-Based Fluorescent Probes to α1-Adrenergic Receptors.
作者信息
Zhang Wei, Ma Zhao, Li Wenhua, Li Geng, Chen Laizhong, Liu Zhenzhen, Du Lupei, Li Minyong
机构信息
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University , Jinan, Shandong 250012, China.
出版信息
ACS Med Chem Lett. 2015 Mar 30;6(5):502-6. doi: 10.1021/ml5004298. eCollection 2015 May 14.
α1-Adrenergic receptors (α1-ARs), as the essential members of G protein-coupled receptors (GPCRs), can mediate numerous physiological responses in the sympathetic nervous system. In the current research, a series of quinazoline-based small-molecule fluorescent probes to α1-ARs (1a-1e), including two parts, a pharmacophore for α1-AR recognition and a fluorophore for visualization, were well designed and synthesized. The biological evaluation results displayed that these probes held reasonable fluorescent properties, high affinity, accepted cell toxicity, and excellent subcellular localization imaging potential for α1-ARs.
α1肾上腺素能受体（α1-ARs）作为G蛋白偶联受体（GPCRs）的重要成员，可介导交感神经系统中的多种生理反应。在当前的研究中，设计并合成了一系列基于喹唑啉的α1-ARs小分子荧光探针（1a-1e），包括两个部分，一个用于识别α1-ARs的药效基团和一个用于可视化的荧光团。生物学评价结果表明，这些探针具有合理的荧光特性、高亲和力、可接受的细胞毒性以及用于α1-ARs的优异亚细胞定位成像潜力。
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